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Duvelisib

IPI 145,INK1197

PI-145 (INK1197)是PI3K δ和γ高度选择性抑制剂,Ki和IC50分别为23 pM/243 pM和1 nM/50 nM。

目录号
EY1701
EY1701
EY1701
EY1701
EY1701
纯度
99.51%
99.51%
99.51%
99.51%
99.51%
规格
1 mg
5 mg
10 mg
50 mg
100 mg
原价
480
1050
1592
5580
8820
售价
480
1050
1592
5580
8820
库存
现货
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm系数


    例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。


  • 参考文献

    [1] Vito Palombella, Targeting PI3K- δ and PI3K-γ in Inflammation, 2012.

    分子式
    C22H17ClN6O
    分子量
    416.86
    CAS号
    1201438-56-3
    储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂(常温)
    DMSO
    80 mg/mL
    Water
    <1 mg/mL
    Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02598570 Lymphoma Drug: duvelisib AbbVie|Infinity Pharmaceuticals, Inc. Phase 1 2015-11-01 2017-02-03
    NCT02095587 Hepatic Impairment Drug: IPI-145 Verastem, Inc. Phase 1 2014-03-01 2017-02-21
    NCT02711852 Hematologic Malignancy Drug: Duvelisib Verastem, Inc. Phase 2 2016-04-01 2017-03-07
    NCT02783625 Lymphoma|Relapsed/Refractory T-cell Lymphomas Drug: Romidepsin|Drug: Bortezomib|Drug: duvelisib Memorial Sloan Kettering Cancer Center|Dana-Farber Cancer Institute|Stanford University Phase 1 2016-05-01 2017-03-02
    NCT02292225 Lymphocytic Leukemia, Chronic|Lymphoma, Small Lymphocytic Drug: IPI-145 (duvelisib)|Drug: Obinutuzumab Verastem, Inc. Phase 1 2015-02-01 2017-02-21
    NCT01882803 Indolent Non-Hodgkin Lymphoma Drug: IPI-145 (duvelisib) Verastem, Inc. Phase 2 2013-05-01 2017-02-21
    NCT02576275 Indolent Non-Hodgkin's Lymphoma|Follicular Lymphoma|Small Lymphocytic Lymphoma|Marginal Zone Lymphoma Drug: Duvelisib|Drug: Placebo|Drug: Rituximab|Drug: Bendamustine Verastem, Inc. Phase 3 2015-12-01 2017-02-21
    NCT02307461 Healthy Drug: IPI-145 (duvelisib)|Drug: IPI-145|Drug: IPI-145 Verastem, Inc. Phase 1 2014-11-01 2017-02-21
    NCT02640833 Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Non-Hodgkin Lymphoma Drug: Duvelisib|Drug: Venetoclax AbbVie|Infinity Pharmaceuticals, Inc. Phase 1 2016-07-01 2016-07-22
    NCT02204982 Follicular Lymphoma Drug: IPI-145 (duvelisib)|Drug: Placebo|Drug: Rituximab Verastem, Inc. Phase 3 2014-09-01 2017-02-21
    NCT02391545 CD20+ Follicular Lymphoma Drug: IPI-145 (duvelisib)|Drug: Rituximab|Drug: Obinutuzumab Verastem, Inc. Phase 1|Phase 2 2014-12-01 2017-03-23
    NCT02004522 Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Drug: IPI-145 (duvelisib)|Drug: Ofatumumab Verastem, Inc. Phase 3 2013-11-01 2017-03-23
    NCT02049515 Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Drug: IPI-145 (duvelisib)|Drug: Ofatumumab Verastem, Inc. Phase 3 2013-12-01 2017-02-21
    NCT01653756 Asthma Drug: IPI-145, a PI3K Inhibitor|Drug: Placebo to match IPI-145 Verastem, Inc. Phase 2 2012-07-01 2017-02-21
    NCT01476657 Hematologic Malignancies Drug: IPI-145 (duvelisib) Verastem, Inc. Phase 1 2011-10-01 2017-02-21
    NCT01836861 Healthy Drug: IPI-145 Verastem, Inc. Phase 1 2013-03-01 2017-02-21
    NCT01549106 Healthy Volunteers Drug: IPI-145|Drug: Placebo Verastem, Inc. Phase 1 2011-08-01 2017-02-21
    NCT01851707 Rheumatoid Arthritis Drug: IPI-145|Drug: Placebo Verastem, Inc. Phase 2 2013-04-01 2017-02-21
    NCT01871675 Lymphoma|Chronic Lymphocytic Leukemia|Non-Hodgkin Lymphoma|T-cell Lymphoma Drug: IPI-145|Drug: Rituximab|Drug: Bendamustine SCRI Development Innovations, LLC|Infinity Pharmaceuticals, Inc. Phase 1 2013-05-01 2016-07-07
    NCT02605694 Lymphoma Drug: Duvelisib|Drug: Rituximab|Drug: R-CHOP|Drug: Prednisone Verastem, Inc. Phase 2 2015-12-01 2017-02-21

    注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。

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